Supramolecular Complex of Ibuprofen with Larch Polysaccharide Arabinogalactan: Studies on Bioavailability and Pharmacokinetics

Хвостов, Михаил В.; Борисов, С. А.; Толстикова, Т. Г.; Душкин, А. В.; Tsyrenova, Biligma D.; Chistyachenko, Yulia S.; Polyakov, Nikolay E.; Dultseva, G.G.; Onischuk, A. A.; An’kov, Sergey V.

doi:10.1007/s13318-016-0357-y

Cited by 25 publications

(5 citation statements)

References 26 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Additionally, evidence of complexation was obtained by NMR relaxation method. The measured relaxation times of the aromatic protons 4-H and m-H in water are 125 ms and 130 ms, which are close in value to the relaxation times of protons of other drug molecules in complexes with AG (ibuprofen, valsartan, etc., 100-140 ms) [35,36]. Due to its low solubility, uncomplexed NIM does not contribute to the observed NMR signal of the complex in water.…”

Section: Inclusion Complex Formation Of Nim From Sd With Polysaccharide Arabinogalactan In Water Solutionmentioning

confidence: 98%

“…In this case, the branched structure of AG macromolecules is especially favorable for complexing drug molecules [8,[33][34][35]. As a result of such complexation the following positive changes in drugs' toxic-pharmacological properties were obtained: increase of water solubility, effective dose and toxic side effects reduction [8][9][10][11]36].…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Solubility, Permeability, Anti-Inflammatory Action and In Vivo Pharmacokinetic Properties of Several Mechanochemically Obtained Pharmaceutical Solid Dispersions of Nimesulide

et al. 2021

Self Cite

View full text Add to dashboard Cite

Nimesulide (NIM, N-(4-nitro-2-phenoxyphenyl)methanesulfonamide) is a relatively new nonsteroidal anti-inflammatory analgesic drug. It is practically insoluble in water (<0.02 mg/mL). This very poor aqueous solubility of the drug may lead to low bioavailability. The objective of the present study was to investigate the possibility of improving the solubility and the bioavailability of NIM via complexation with polysaccharide arabinogalactan (AG), disodium salt of glycyrrhizic acid (Na2GA), hydroxypropyl-β-cyclodextrin (HP-β-CD) and MgCO3. Solid dispersions (SD) have been prepared using a mechanochemical technique. The physical properties of nimesulide SD in solid state were characterized by differential scanning calorimetry and X-ray diffraction studies. The characteristics of the water solutions which form from the obtained solid dispersions were analyzed by reverse phase and gel permeation HPLC. It was shown that solubility increases for all complexes under investigation. These phenomena are obliged by complexation with auxiliary substances, which was shown by 1H-NMR relaxation methods. The parallel artificial membrane permeability assay (PAMPA) was used for predicting passive intestinal absorption. Results showed that mechanochemically obtained complexes with polysaccharide AG, Na2GA, and HP-β-CD enhanced permeation of NIM across an artificial membrane compared to that of the pure NIM. The complexes were examined for anti-inflammatory activity on a model of histamine edema. The substances were administered per os to CD-1 mice. As a result, it was found that all investigated complexes dose-dependently reduce the degree of inflammation. The best results were obtained for the complexes of NIM with Na2GA and HP-β-CD. In noted case the inflammation can be diminished up to 2-fold at equal doses of NIM.

show abstract

Section: Inclusion Complex Formation Of Nim From Sd With Polysaccharide Arabinogalactan In Water Solutionmentioning

confidence: 98%

Section: Introductionmentioning

confidence: 99%

Solubility, Permeability, Anti-Inflammatory Action and In Vivo Pharmacokinetic Properties of Several Mechanochemically Obtained Pharmaceutical Solid Dispersions of Nimesulide

et al. 2021

Self Cite

View full text Add to dashboard Cite

show abstract

“…The Cmax of IBU at doses of 20 and 40 mg/kg was found as 0.088 and 0.132 μg/mL, respectively, while the Cmax of IBU in the complex form was 0.103 and 0.160 μg/mL, respectively. Thus, the complexation of IBU with AG results in an increase in its bioavailability and reduction in the effective dose, which should decrease toxic side effects [ 115 ].…”

Section: Overview On Polysaccharide-based Drug Delivery Systemsmentioning

confidence: 99%

Polysaccharide-Based Coatings as Drug Delivery Systems

Visan,

Cristescu

2023

Pharmaceutics

View full text Add to dashboard Cite

Therapeutic polysaccharide-based coatings have recently emerged as versatile strategies to transform a conventional medical implant into a drug delivery system. However, the translation of these polysaccharide-based coatings into the clinic as drug delivery systems still requires a deeper understanding of their drug degradation/release profiles. This claim is supported by little or no data. In this review paper, a comprehensive description of the benefits and challenges generated by the polysaccharide-based coatings is provided. Moreover, the latest advances made towards the application of the most important representative coatings based on polysaccharide types for drug delivery are debated. Furthermore, suggestions/recommendations for future research to speed up the transition of polysaccharide-based drug delivery systems from the laboratory testing to clinical applications are given.

show abstract

“…Arabinogalactan is biodegradable, biocompatible and hydrophilic, contains different functional groups such as hydroxyl, carboxylic acid, that make it ideal for conjugation and delivery of carotenoids and drug molecules. There are many examples of increased solubility of hydrophobic drugs in the complexes with AG [72,73,74]. Some recent studies indicate also that AG has good adhesion to membrane surface, and is able to enhance the membrane permeability for both human and plant cell membranes [21,75].…”

Section: Inclusion Complexesmentioning

confidence: 99%

Supramolecular Carotenoid Complexes of Enhanced Solubility and Stability—The Way of Bioavailability Improvement

2019

View full text Add to dashboard Cite

Carotenoids are natural dyes and antioxidants widely used in food processing and in therapeutic formulations. However, their practical application is restricted by their high sensitivity to external factors such as heat, light, oxygen, metal ions and processing conditions, as well as by extremely low water solubility. Various approaches have been developed to overcome these problems. In particular, it was demonstrated that application of supramolecular complexes of “host-guest” type with water-soluble nanoparticles allows minimizing the abovementioned disadvantages. From this point of view, nanoencapsulation of carotenoids is an effective strategy to improve their stability during storage and food processing. Also, nanoencapsulation enhances bioavailability of carotenoids via modulating their release kinetics from the delivery system, influencing the solubility and absorption. In the present paper, we present the state of the art of carotenoid nanoencapsulation and summarize the data obtained during last five years on preparation, analysis and reactivity of carotenoids encapsulated into various nanoparticles. The possible mechanisms of carotenoids bioavailability enhancement by multifunctional delivery systems are also discussed.

show abstract

Supramolecular Complex of Ibuprofen with Larch Polysaccharide Arabinogalactan: Studies on Bioavailability and Pharmacokinetics

Abstract: Thus, we have shown that complexation of the IBU with AG results in its bioavailability increase, reduction of the effective dose and should decrease toxic side effects.

Cited by 25 publications

References 26 publications

Solubility, Permeability, Anti-Inflammatory Action and In Vivo Pharmacokinetic Properties of Several Mechanochemically Obtained Pharmaceutical Solid Dispersions of Nimesulide

Solubility, Permeability, Anti-Inflammatory Action and In Vivo Pharmacokinetic Properties of Several Mechanochemically Obtained Pharmaceutical Solid Dispersions of Nimesulide

Polysaccharide-Based Coatings as Drug Delivery Systems

Supramolecular Carotenoid Complexes of Enhanced Solubility and Stability—The Way of Bioavailability Improvement

Contact Info

Product

Resources

About